Issue 14, 2018

A long-lived cuprous bis-phenanthroline complex for the photodynamic therapy of cancer

Abstract

Copper is an earth-abundant and a biologically essential metal that offers a promising alternative to noble metals in photochemistry and photobiology. In this work, a series of sterically encumbered Cu(I) bis-phenanthroline complexes were investigated for their use in photochemotherapy (PCT). It was found that Cu(dsbtmp)2+ [dsbtmp = 2,9-disec-butyl-3,4,7,8-tetramethyl-1,10-phenanthroline] (compound 3), which possessed the longest excited state lifetime, exhibited significant in vitro photocytotoxicity on A375 (human malignant melanoma) and A549 (human lung carcinoma) cell lines. Fluorescence imaging demonstrated the significant uptake and localization of compound 3 in a perinuclear fashion. A comet assay indicated the induction of DNA damage in the dark. The DNA breaks were significantly amplified upon photoactivation. The light-induced enhancement of cytotoxicity was associated with the formation of reactive oxygen species (ROS), a known intermediate in photodynamic therapy (PDT). This successful demonstration of photocytotoxicity using long-lived cuprous phenanthroline paves the way to exploit this class of photosensitizers for PDT applications.

Graphical abstract: A long-lived cuprous bis-phenanthroline complex for the photodynamic therapy of cancer

Supplementary files

Article information

Article type
Paper
Submitted
11 Janv. 2018
Accepted
27 Febr. 2018
First published
27 Febr. 2018
This article is Open Access
Creative Commons BY-NC license

Dalton Trans., 2018,47, 4959-4967

A long-lived cuprous bis-phenanthroline complex for the photodynamic therapy of cancer

C. Al Hageh, M. Al Assaad, Z. El Masri, N. Samaan, M. El-Sibai, C. Khalil and R. S. Khnayzer, Dalton Trans., 2018, 47, 4959 DOI: 10.1039/C8DT00140E

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